选择性和竞争性 P2Y2 拮抗剂
Selective, competitive P2Y2 receptor antagonist. Inactive against a panel of 37 other receptors at a concentration of 10 μM. Inhibits ATP-γS-induced mucin secretion in bronchial epithelial cells (IC50 = 1 μM). Inhibits P2Y2 receptor-induced β-arrestin translocation in vitro (pA2 = 37.2-51.3 nM).
Reference:
Kemp et al (2004) Nucleotide-mediated mucin secretion from differentiated human bronchial epithelial cells. Am.J.Respir.Cell Mol.Biol. 31 446 PMID:15231488
Meghani (2002) The design of P2Y2 antagonists for the treatment of inflammatory diseases. Abstract of papers, 224th ACS National Meeting, Boston, MA
Rafehi et al (2017) Synthesis, characterization, and in vitro evaluation of the selective P2Y2 receptor antagonist AR-C118925. Purinergic.Signal. 13 89 PMID:27766552
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